Target
Glutaminase kidney isoform, mitochondrial
Ligand
BDBM404908
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
<100±n/a nM
Citation
 Di Francesco, MEJones, PHeffernan, THamilton, MMKang, ZSoth, MJBurke, JPLe, KCarroll, CLPalmer, WSLewis, RMcAfoos, TCzako, BLiu, GTheroff, JHerrera, ZYau, A GLS1 inhibitors for treating disease US Patent  US10344025 Publication Date 7/9/2019 
Target
Name:
Glutaminase kidney isoform, mitochondrial
Synonyms:
GLS | GLS1 | GLSK_HUMAN | Glutaminase 1 | K-glutaminase | KIAA0838 | L-glutamine amidohydrolase
Type:
Protein
Mol. Mass.:
73471.89
Organism:
Homo sapiens (Human)
Description:
O94925
Residue:
669
Sequence:
MMRLRGSGMLRDLLLRSPAGVSATLRRAQPLVTLCRRPRGGGRPAAGPAAAARLHPWWGGGGWPAEPLARGLSSSPSEILQELGKGSTHPQPGVSPPAAPAAPGPKDGPGETDAFGNSEGKELVASGENKIKQGLLPSLEDLLFYTIAEGQEKIPVHKFITALKSTGLRTSDPRLKECMDMLRLTLQTTSDGVMLDKDLFKKCVQSNIVLLTQAFRRKFVIPDFMSFTSHIDELYESAKKQSGGKVADYIPQLAKFSPDLWGVSVCTVDGQRHSTGDTKVPFCLQSCVKPLKYAIAVNDLGTEYVHRYVGKEPSGLRFNKLFLNEDDKPHNPMVNAGAIVVTSLIKQGVNNAEKFDYVMQFLNKMAGNEYVGFSNATFQSERESGDRNFAIGYYLKEKKCFPEGTDMVGILDFYFQLCSIEVTCESASVMAATLANGGFCPITGERVLSPEAVRNTLSLMHSCGMYDFSGQFAFHVGLPAKSGVAGGILLVVPNVMGMMCWSPPLDKMGNSVKGIHFCHDLVSLCNFHNYDNLRHFAKKLDPRREGGDQRVKSVINLLFAAYTGDVSALRRFALSAMDMEQRDYDSRTALHVAAAEGHVEVVKFLLEACKVNPFPKDRWNNTPMDEALHFGHHDVFKILQEYQVQYTPQGDSDNGKENQTVHKNLDGLL
  
Inhibitor
Name:
BDBM404908
Synonyms:
1-(4-(6-(2-(4-(3,3- difluorocyclobutoxy)pyridin-2- yl)acetamido)pyridazin-3-yl)-2- fluorobutyl)-N-methyl-1H-1,2,3- triazole-4-carboxamide | US10344025, Example 252 | US11370786, Example 252
Type:
Small organic molecule
Emp. Form.:
C23H25F3N8O3
Mol. Mass.:
518.4916
SMILES:
CNC(=O)c1cn(CC(F)CCc2ccc(NC(=O)Cc3cc(OC4CC(F)(F)C4)ccn3)nn2)nn1
Structure:
Search PDB for entries with ligand similarity: